Relivyx Plus (lidocaine/menthol)

Topical Local Anesthetics Topical Kit

Advertisement

Last reviewed · Source: First Databank (FDB) drug data

Overview

Lidocaine, a nonselective voltage-gated sodium channel inhibitor, is an amide-type local anesthetic.

Lidocaine is an amide-type local anesthetic that blocks sodium ion channels required for the initiation and conduction of neuronal impulses. The analgesic effects of lidocaine are thought to result from these effects. Penetration of lidocaine into intact skin is sufficient to produce an analgesic effect; however, the amount is insufficient to produce a complete sensory block.

Ztlido(R) (lidocaine topical system) 1.8% is a single-layer, drug-in-adhesive, topical deliverysystem comprised of an adhesive material containing 36 mg lidocaine, which is applied toa pliable nonwoven cloth backing and covered with a polyethylene terephthalate (PET) filmrelease liner. Lidoderm(R) transdermal patch is composed of an adhesive material containing 5%lidocaine, which is applied to a nonwoven polyester felt backing and covered with aPET film release liner. The release liner is removed prior toapplication of both the Ztlido(R) and Lidoderm(R) patches.

The amount of lidocaine that is systemically absorbed from a lidocaine patch is directly related toboth the duration of application and the surface area over which it is applied. There is minimal systemic absorption (approximately 3%) when the 5% patches are used topically as recommended and maximum blood concentrations are about 1/10 of the therapeutic concentration required to treat cardiac arrhythmias. In apharmacokinetic study evaluating lidocaine 5% patches, 3 patches (total of 2100 mg) were applied over an area of 420 cm2of intact skin on the backs of normal volunteers for 12 hours.

The total dose absorbed was approximately 64 mg and time to peak plasma concentration was 11 hours. Mean lidocaine blood concentrations after 3 consecutive days of daily use (3 patches applied at the same time for 12 hours once daily for 3 days) remained the same. In a pharmacokinetic study evaluating the 1.8% patches, 3 patches (total dose of 108 mg) were applied over an area of 420 cm2of intact skin on the backs of normal volunteers for 12 hours.

Time to peak plasma concentration was approximately 14 hours. Mean lidocaine blood concentrations after 3 consecutive days of daily use (3 patches applied at the same time for 12 hours once daily for 3 days) remained the same.

Lidocaine is approximately 70% bound to plasma proteins (primarily alpha-1-acid glycoprotein) at concentrations achieved from topical application; at higher concentrations, plasma protein binding is concentration dependent. Lidocaine crosses the placental and blood brain barriers, presumably by diffusion. It is not known if lidocaine is metabolized in the skin.

However, lidocaine is extensively metabolized in the liver to several pharmacologically active metabolites and is excreted by the kidneys (less than 10% as unchanged drug).

Lidocaine 1.8% patches (Ztlido(R)) are bioequivalent to lidocaine 5% patches (Lidoderm(R) and generics).

Lidocaine is used topically for the treatment of pain. Various topical lidocaine products are commercially available. Lidocaine 1.8% and 5% topical systems (i.e., patches) are FDA-labeled for the treatment of pain associated with postherpetic neuralgia (PHN).

Lidocaine is also available in various over-the-counter (OTC) topical preparations for the temporary treatment of pain.

Generic name: lidocaine/menthol
Drug class: Topical Local Anesthetics
Therapeutic class: Dermatological

Reference product & biosimilars

No reference, biosimilar or interchangeable associated with this drug.

Today’s intelligence on Relivyx Plus

Intelligence content is not available yet.

Indications

No indications are available for this drug.

Dosing

No dosing information is available for this tab.

Drug interactions

There is no enhanced messaging for this drug.

Contraindications

*Known history of sensitivity to local anesthetic of the amide type, or to any other component of the product.

Adverse reactions

Common adverse effects of lidocaine 1.8 and 5% patches include mild and transient application site reactions (e.g., blisters, bruising, burning sensation, depigmentation,dermatitis, discoloration, edema, erythema, exfoliation, irritation, papules, petechia,pruritus, vesicles).

Systemic adverse reactions following topical use of lidoderm patch are unlikely due to minimal drug absorption.

Precautions

No enhanced messaging available.

ICD codes

No ICD codes are available for this drug.

Formulary status

Search health-plan coverage for this drug by ZIP code.

Enter a ZIP code to view available health plans.

Last reviewed · Source: First Databank (FDB) drug data